- COMPOUNDS
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Disclosed are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis(ALS).
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- 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists
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As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT6 receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT6 antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.
- Liu, Kevin G.,Robichaud, Albert J.,Bernotas, Ronald C.,Yan, Yinfa,Lo, Jennifer R.,Zhang, Mei-Yi,Hughes, Zoe A.,Huselton, Christine,Zhang, Guo Ming,Zhang, Jean Y.,Kowal, Dianne M.,Smith, Deborah L.,Schechter, Lee E.,Comery, Thomas A.
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scheme or table
p. 7639 - 7646
(2011/02/21)
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- 6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 34; 36
(2008/12/08)
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- Heterocyclyl-3-sulfonylindazoles as 5-hydroxytryptamine-6 ligands
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The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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Page/Page column 22-23
(2008/06/13)
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